Synfacts

Issue 07 · July 2022

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A101
SYNFORM ISSUE 2022/07 FREE ACCESS

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Synthesis of Natural Products and Potential Drugs
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0703
Total Synthesis of (–)-Phaeocaulisin A FREE ACCESS

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0704
Iridium-Catalyzed Asymmetric Hydrogenation of an Indenopyridine: 11β-HSD-1 Inhibitor

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0705
Synthesis of a Respiratory Syncytial Virus Drug Candidate

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0706
Total Synthesis of (+)-Elansolid A

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0707
Synthesis of (+)-Cochlearol B

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0708
Formal Synthesis of PF-06873600

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0709
Total Synthesis of (±)-Ocellatusone C

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0710
Synthesis of Roxadustat

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0711
Synthesis of Verinurad

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0712
Synthesis of Antimalarial BRD5018

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0713
Synthesis of a Farnesoid X Receptor Agonist

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0714
Large-Scale Synthesis of the 2′-C-Methyluridine Core of Uprifosbuvir

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0715
Asymmetric Total Synthesis of (2R)-Hydroxynorneomajucin

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0716
Synthesis of Upadacitinib

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0717
Synthesis of QPX7728

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0718
Synthesis of (+)-Decursivine

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0719
Synthesis of (±)-Quadrone FREE ACCESS

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0720
Synthesis of BACE1 Inhibitor E2609 (Elenbecestat)

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Synthesis of Heterocycles
z0721
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0721
Preparation of 2-Aminopyridines and 2-Aminoazines by a Zincke Reaction

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0722
Expeditious Robust Elaboration of Bicyclic N-Heterocycles

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0723
Gram-Scale Synthesis of Fluorinated Pyrazoles and Pyridines

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0724
Regioselective Functionalization of in situ Generated Heteroaryl Grignards with Tosyl Aziridines

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0725
Gold/Iridium-Catalyzed Enantioselective Synthesis of Spiroketals and Spiroaminals

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0726
Gold-Catalyzed Asymmetric Annulations of Enynone Derivatives and Nitrones Generated In Situ

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0727
TEMPO Salt Mediated Oxidative Ugi–Azide Approach to Direct Functionalization of N-Heterocycles

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0728
BINOL-Mediated Asymmetric Synthesis of Ammonium Salts

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0729
Photocatalytic Conversion of Indoles into Spirocyclic Indolines

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0730
Organophotoredox-Catalyzed Synthesis of Benzazepine Derivatives under Benign Conditions

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0731
Tertiary Amines by Palladium-Mediated Allylic C–H Amination

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0732
Copper-Catalyzed Borylation of (Het)aryl Carboxylic Acids

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0733
Construction of Silicon Heterocycles by Cobalt-Catalyzed Hydrosilylation of Enynes

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Synthesis of Materials and Unnatural Products
z0735
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0735
Picene Together a Geodesic Polyarene

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0736
Heptagon-Embedded Monkey-Saddle-Shaped Nanographene via Photocyclization

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0737
Thinking Inside the BOX for Helical, Isotactic Poly(NVC)s

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0738
An Orthogonal Approach to Neutral Diradicals

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0739
Treble Triptycenes, Triple the Thrill

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0740
An Easy Prep for Triphenylenes

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0741
Copper-Mediated Fullerooxazoles Synthesis

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0742
Design of Bright Curved Dyes

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0743
Flattened Triarylboranes

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0744
Synthesis of Bibenzothiophene from Arylthiol and 1,3-Diynes

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0745
Synthesis of C8-Aminated Pyrrolo-Phenanthridines or -Indoles via C–H Activation

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0746
COF Remodeling

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Metals in Synthesis
z0747
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0747
Take Two CO: Access to γ-Boryl Esters by Boration and Carbonylative Catenation of Styrenes in One Pot FREE ACCESS

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0748
Ruthenium-Catalyzed Direct Asymmetric Reductive Amination of α-Keto Amides with Ammonium Salts

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0749
Photoinduced Cobalt-Catalyzed Enantioselective Reductive Addition of Aryl Iodides to Aldehydes FREE ACCESS

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0750
1,2-Alkylsulfenylation and -Selenolation of Alkenes with Organozinc Nucleophiles

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0751
A Mild Nickel-Catalyzed Protocol for the α-Arylation of Amides Using Redox-Active Esters

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0752
Kumada–Tamao–Corriu Cross-Coupling by Rhodium–Aluminum Cooperative Catalysis

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0753
Nickel-Catalyzed C(sp³)–H Functionalization with Organohalides by Thermal Redox Coupling

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0754
Enantioselective Arylborylation of Alkenes Catalyzed by Palladium

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0755
Dearomative C2-Alkylation of Indoles Using Nickel Catalysis

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0756
Asymmetric Synthesis of Dihydropyranes through a Catalytic Hetero-Diels–Alder Reaction

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0757
New Electrophilic Sulfur Reagent and its Application in a Ni-Catalyzed syn-Carbosulfenylation of Alkenes

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0758
Aminocarbonylation of Ethers under Cobalt Catalysis

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0759
Stereoselective α-Alkylation of Esters with Oxyallenes Using Cooperative Catalysis

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0760
A Palladium-Catalyzed Dearomative Carbonylation Approach to Polycyclic Indolines

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0761
Co/Salox Catalyzed C–H Annulation of Arylphosphinamides with Alkynes and Allenes

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0762
Synthesis of Aryl Nitriles by a Nickel-Catalyzed Aryl Exchange Reaction

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0763
Hydrazone–Olefin and Oxime–Olefin Ring-Closing Metathesis

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0764
Stuck Together! Acetylene as Molecular Glue for the Synthesis of Ethylene-Linked Functionalized Ketones

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0765
One Out of Two! Selective Deoxygenative Reduction of 1,3-Diketones under Rhodium Catalysis

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0766
Synthesis of Benzimidazolones and Benzimidazoles via Copper-Catalyzed C–H Amination/Annulation Cascade

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0767
Amide-Directed Regioselective Hydroalkylation of Unactivated Alkenes under Nickel Hydride Catalysis

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0768
Gold-Catalyzed Enantioselective Aminoarylation of Olefins

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0769
Palladium-Catalyzed Desymmetrization of Olefins via Heck–Matsuda Coupling with Anilines

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0770
Accessing 1,1-Diarylalkanes via a Ruthenium-Catalyzed meta-Selective C–H Functionalization

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0771
Accessing Trimethylenemethane-Palladium Complexes with 2-Acetoxymethyl-3-allyltrimethylsilane FREE ACCESS

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0772
The Chan–Evans–Lam Coupling FREE ACCESS

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Polymer-Supported Synthesis
z0773
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0773
Ammoxidation of Alcohols with Aqueous Ammonia Using an Iron Single-Atom Catalyst

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0774
Synthesis of Trisubstituted Imidazoles by Sulfonated Magnetic Cellulose-Nanoparticles

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0775
Hydrothiolation of Alkenes and Alkynes on Carbon Nanotube-Supported Ru–Rh Nanoparticles

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0776
Willgerodt–Kindler Reaction on Supported Silver Nanoparticles

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0777
Asymmetric Aldol Reaction Catalyzed by a Chiral Proline-Substituted Porous Organic Cage

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0778
Hydrolytic Oxidation of Hydrosilanes on PtCu Nanowires Encapsulated in Ir(III) Porphyrinic MOFs

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0779
Hydrodeoxygenation of Lignin Derivatives Catalyzed by Kieselguhr-Supported Palladium Nanoparticles

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0780
Suzuki–Miyaura and Ullmann Couplings of Aryl Chlorides Catalyzed by Silk-Fibroin-Supported Pd

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0781
Reductive N-Alkylation of Amines with Aldehydes and Ketones on a Zirconia-Supported Pd Catalyst

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0782
Hydrodeoxygenation of Acetophenone Derivatives on a an Iron–Ruthenium Bimetallic Catalyst

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0783
Photocatalytic Cross-Coupling of Alkyl Silicates with Aryl or Alkenyl Bromides

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Organo- and Biocatalysis
z0785
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0785
Multifunctional Biocatalyst for Iminium-Activated Conjugate Reduction/Reductive Amination

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0786
Chiral Hexameric Resorcin[4]arene Capsules Enable Asymmetric Tail-to-Head Terpene Cyclizations

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0787
Energy-Transfer-Induced Strain-Release [2π+2σ] Cycloadditions FREE ACCESS

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0788
Stereoselective Dearomatizing Diels–Alder Reaction to Construct Complex Polycyclic Compounds

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0789
Hydrazine-Catalyzed Ring-Opening Carbonyl–Olefin Metathesis between Cyclobutenes and Aldehydes

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0790
Enantioselective Reactions of Primary Radicals Catalyzed by Engineered Ketoreductases

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0791
Asymmetric Aldol Condensation Enables Diastereodivergent Synthesis of Two-Axis Atropisomers

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0792
NHC-Catalyzed Intramolecular S_NAr Reaction of Styrenes for the Synthesis of Polyaromatic Compounds

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0793
Cooperative Photoredox and Chiral Hydrogen-Bonding Catalysis Enables Enantioselective Radical Coupling

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0794
1,3,2-Diazaphospholene Catalyst Enables Reductive Cyclizations of Organohalides

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0795
Dual Lewis Base and Photoredox Catalysis Permits the Enantioselective Synthesis of Pyrrolidinones

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0796
Visible-Light-Driven Organocatalytic Radical Addition to Imines

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Chemistry in Medicine and Biology
z0797
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0797
A Natural Product Hybrid with Potent Antitumor Activity

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0798
Breaking the Mirror: Deracemization of α-Branched Aldehydes

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0799
Harnessing the Power of Organo- and Biocatalysis to Synthesize STING Agonist MK-1454

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0800
Unexpected Hydrolytic Triazoloquinazoline Ring Opening Leads to a Potent HDAC6 Inhibitor

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0801
Expanding the E3 Ligase Toolbox by Co-opting Methyl Readers

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0802
Novel Macrocycle-Based Type-II TRK Inhibitors

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0803
A Rapid Approach to Cyclopropane-Fused Lactams

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0804
Tuning Colors of the Drug: A Systematic Study of the Emissive Features of the Deferasirox Scaffold

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0805
A Reversible Covalent Inhibitor Targeting the BCR-ABL Active-Site Lysine

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0806
Fluorogenic Cyclopropenones for Cellular Imaging

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0807
An Improved Orthosteric Antagonist of the M₅ Muscarinic Acetylcholine Receptor

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0808
A Diastereoselective Cyclopropanation Strategy

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0809
The First Total Synthesis of Bryostatin 7 FREE ACCESS

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Peptide Chemistry
z0811
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0811
1,2-Diaminotruxinic Bis-amino Acid Synthesis

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0812
Site-Selective Replacement of N-Protecting Groups in Peptides

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0813
A Novel Reagent for Coupling of Amino Acid Chlorides with Amino Acid Esters FREE ACCESS

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0814
Lewis Acid/Palladium-Catalyzed Synthesis of α-Amino Acid Derivatives

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0815
Synthesis of Carborane-Decorated Tryptophan-Containing Peptides

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0816
Nickel/Copper-Catalyzed Synthesis of Tetrasubstituted Amino Acids

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0817
Copper-Catalyzed Cross-Dehydrogenative Coupling for Amino Acid and Peptide Synthesis

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0818
Synthesis of Functionalized and Macrocyclic Peptides by C–H Olefination FREE ACCESS

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0819
α-Trifluoromethyl Amino Acid Synthesis by a Biocatalytic N–H Carbene Insertion

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Flow Chemistry
z0821
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0821
Electrochemical Oxidation of Primary Alcohol in Single-Pass Continuous Flow

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0822
Photochemical Synthesis of Alkyl Zinc Sulfinates under Flow Conditions

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0823
Aerobic Oxidations of Aldehydes in Continuous Flow Catalyzed by N-Hydroxyphthalimide

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